Kk. Peh et Kh. Yuen, STEADY-STATE PHARMACOKINETICS OF A MULTIPARTICULATE MATRIX SUSTAINED-RELEASE THEOPHYLLINE PREPARATION, Drug development and industrial pharmacy, 22(11), 1996, pp. 1133-1138
A novel multiparticulate matrix sustained-release theophylline prepara
tion was evaluated in comparison with a reference product, Neulin-SR(R
), in a multiple-dose administration study, conducted according to a r
andomized, two-way crossover design involving 12 healthy volunteers. C
omparison was made using the parameters, area under the serum concentr
ation-time curve from time 0 to 12 hr (AUC(0-12)), time to reach peak
serum concentration (T-max), peak serum concentration (C-max), trough
serum concentration (C-min), average drug concentration (C-av), degree
of fluctuation (DF), percentage of time serum drug concentrations lie
within the therapeutic range (occupancy time) and time for 50% of dos
e absorbed (T-50%). The parameters, C-max, C-min, AUC(0-12), C-av, and
DF were logarithmic transformed prior to statistical analysis. A stat
istically significant difference was obtained between the values of th
e two preparations in the T-max, C-min, DF, and T-50%; but not in the
C-max, AUC(0-12), C-av, and occupancy time. These findings suggest tha
t the novel preparation has a more sustained rate but equivalent exten
t of absorption compared to Neulin-SR, leading to a more uniform stead
y-state serum profile.